Tipifarnib

Product Name: Tipifarnib
CAS No.: 192185-72-1
Chemical Name: Tipifarnib
Synonyms: CS-2330;R115777;IND 58359;Zarnestra;ipifarnib;TIPIFARNIB;(R)-(+)-R 115777;Tipifarnib(R115777);TIPIFARNIB ZARNESTRA;Tipifarnib USP/EP/BP
CBNumber: CB61011759
Molecular Formula: C27H22Cl2N4O
Formula Weight: 489.4
MOL File: 192185-72-1.mol

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Tipifarnib Property

Melting point:: 211-213°C (dec.)
Boiling point:: 681.7±55.0 °C(Predicted)
Density: 1.33±0.1 g/cm3(Predicted)
storage temp.: -20°C
solubility: Chloroform (Slightly), Methanol (Slightly)
pka: 7.20±0.10(Predicted)
form: powder
color: white to beige
optical activity: [α]/D 17 to 24°, c = 1 in methanol

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Safety

HS Code: 2933790090

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1668
Product name: Tipifarnib
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $131
Updated: 2023/06/20

Sigma-Aldrich

Product number: SML1668
Product name: Tipifarnib
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $530
Updated: 2023/06/20

Cayman Chemical

Product number: 11747
Product name: Tipifarnib
Purity: ≥98%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 11747
Product name: Tipifarnib
Purity: ≥98%
Packaging: 5mg
Price: $118
Updated: 2024/03/01

Cayman Chemical

Product number: 11747
Product name: Tipifarnib
Purity: ≥98%
Packaging: 10mg
Price: $214
Updated: 2024/03/01

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Tipifarnib Chemical Properties,Usage,Production

Chemical Properties

Off-White to Pale Beige Solid

Uses

A farnesyltransferase inhibitor. Sensitizes human multiple myeloma cell to proteasome inhibition by blocking degradation of bortezomib(B675700)-induced aggresomes. Also shown to inhibit the growth of myeloid leukemia cell lines and primary leukemia cells by inducing apoptosis and cell-cycle blockage when combined with rapamycin(R124000).

Definition

ChEBI: Tipifarnib is a quinolone that is 1-methylquinolin-2-one which carries a 3-chlorophenyl and an amino(4-chlorophenyl)(1-methyl-imidazol-5-yl)methyl groups at the 4 and 6 positions, respectively (the R-isomer). It has a role as an antineoplastic agent, an EC 2.5.1.58 (protein farnesyltransferase) inhibitor and an apoptosis inducer. It is a quinolone, a member of monochlorobenzenes, a member of imidazoles and a primary amino compound.

General Description

Pre-clinical studies show that tipifarnib has antiproliferative effects on pancreatic cancer cell lines at clinically relevant concentrations (concentration that inhibits 50% growth [IC50] from 9.5 to 500?nmol/L). It also exhibits marked growth retardation and antiangiogenic effects in a pancreatic cancer xenograft model.

Biological Activity

tipifarnib (also known as zarnestra or r115777), an orally bioavailable quinolone analog of imidazole heterocyclics, is a potent and specific nonpeptidomimetic competitive inhibitor of farnesyltransferase (ftase), an enezyme mediating post-translational farnesylation of multiple protein substrates involved in tumor cell proliferation. it has demonstrated inhibition of growth and proliferation of a broad range of human tumor models (either wild-type or mutated ras) via cytostatic rather than cytotoxic activity both in vitro and in vivo. it cell-type dependently induces apoptosis in some neoplastic cell lineages other than acute myeloid leukemia (aml), including multiple myeloma (mm) cell lines and mm cultures from patients.p.k. epling-burnett and thomas p. loughran jr. suppression of farnesyltransferase activity in acute myeloid leukemia and myelodysplastic syndrome: current understanding and recommended use of tipifarnib. expert opin investig drugs. 2010; 19(5): 689-698jean-pierre armand, alan k. burnett, johannes drach, jean-luc harousseau, bob lowenberg and jesus san miguel. the emerging role of targeted therapy for hematologic malignancies: update on bortezomib and tipifarnib. the oncologist 2007, 12:281-290elzbieta izbicka, david campos, gilbert carrizales and amita patnaik. biomarkers of anticancer activity of r115777 (tipifarnib, zarnestra) in human breast cancer models in vitro. anticancer research 2005; 25: 3215-3224

Biochem/physiol Actions

Tipifarnib (R115777) is an orally active and potent farnesyltransferase (FTase) inhibitor that exhibits potent anti-tumorigenic effects. Tipifarnib mechanism of action is not fully understand.

target

FTase

Tipifarnib Preparation Products And Raw materials

Raw materials

Preparation Products

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Tipifarnib Suppliers

Canada 1 China 124 India 3 United Kingdom 3 United States 21 Global 152

LGM Pharma

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View Lastest Price from Tipifarnib manufacturers

Career Henan Chemical Co

Product: Tipifarnib 192185-72-1
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-23

192185-72-1, TipifarnibRelated Search:

Glucosamine Levamisole Methylparaben Sulfamic acid Thiophanate-methyl Bensulfuron methyl Methyl acrylate EC 2.6.1.2 Methyl acetate Imidazole FARNESOL Acetaminophen Kresoxim-methyl Methyl FARNESENE (MIXTURE OF ISOMERS)[FOR PERFUMERY] Phenylacetone Methyl bromide Parathion-methyl

ipifarnib

CS-2330

ZARNESTRA; IND 58359; R115777; IND-58359; IND58359; R-115777; R 115777

TIPIFARNIB

TIPIFARNIB ZARNESTRA

(R)-6-(Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone

Zarnestra

(R)-(+)-R 115777

6-[(R)-AMino(4-chlorophenyl)(1-Methyl-1H-iMidazol-5-yl)Methyl]-4-(3-chlorophenyl)-1-Methyl-2(1H)-quinolinone

Tipifarnib(Zarnestra,NSC-702818, R-115777)

IND 58359

R115777

Tipifarnib(R115777)

(R)-6-(amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one

Tipifarnib (Zarnestra) IND 58359, R115777

Tipifarnib (IND 58359

2(1H)-Quinolinone, 6-[(R)-amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-

Tipifarnib USP/EP/BP

6-[(R)-amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one

192185-72-1

192185-71-4

Inhibitors

Amines

Aromatics

Heterocycles

Intermediates & Fine Chemicals

Pharmaceuticals

Tyrosine Kinase Inhibitors

Inhibitor

Antineoplastic